1. Field of the Invention:
This invention embodies new and novel compounds useful as analgesics and/or narcotic antagonists and a new and novel total synthesis for their preparation.
2. Description of the Prior Art:
A. Everette May and Hiroshi Kugita, J. Org. Chem. 26, 188 (1961) describe compounds having the formula ##SPC1##
In which R.sub.2 is H or methyl and R is methyl or phenethyl as being moderate to weak analgetics.
B. Everette May, James Murphy and J. Harrison Ager, J. Org. Chem. 25, 1386 (1960) report compounds having the formula ##SPC2##
In which R is methyl or phenethyl and R.sup.2 is H or methyl as being potent analgetics.
C. Everette May, Hiroshi Kugita and J. Harrison Ager, J. Org. Chem. 26, 1621 (1961) report compounds having the formula ##SPC3##
In which R is methyl or phenethyl, R.sup.1 is methyl or H, R.sup.3 is H, OH or methoxy as producing varying degrees of analgesia.
D. Everette May, Colin Chignell and J. Harrison Ager, J. Med. Chem. 8, 235 (1965) report compounds having the formula ##SPC4##
In which R.sup.1 is H or methyl and R.sup.2 is methyl as possessing analgetic activity.
E. Everette May and Hiroshi Kugita, J. Org. Chem. 26 1954 (1961) report the compound having the formula ##SPC5##
In which R is methyl or phenethyl, R.sup.1 is H or methyl and R.sup.2 is H or acetyl as having analgetic activity.
F. Everette May and Seiichi Sato, J. Org. Chem. 26, 4536 (1961) report compounds having the formula ##SPC6##
In which R.sup.2 is H or methyl, R.sup.1 is methyl or ethyl, R.sup.3 is methyl or ethyl and R.sup.4 is H or acetyl as possessing analgetic activity.
G. N. B. Eddy and E. L. May published a review of 6,7-benzomorphans in Synthetic Analgetics, Pergamon Press (1966).